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428205 Lck Inhibitor - CAS 213743-31-8 - Calbiochem

428205
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Overview

Key Spec Table

CAS #Empirical Formula
213743-31-8C₂₃H₂₂N₄O

Products

Catalogue NumberPackaging Qty/Pack
428205-1MG Plastová ampulka 1 mg
Description
OverviewA cell-permeable pyrrolopyrimidine compound that acts as a potent, reversible, selective, and ATP-competitive inhibitor of Lck (IC50 at 5 µM ATP = < 1 nM, 2 nM, 70 nM, 1.57 µM and 1.98 µM for lck64-509 Y394, Lckcd pY394, Src, Kdr and Tie-2, respectively; IC50 at 1 mM ATP = 16 µM, 66 nM, 126 nM, 420 nM and 5.18 µM for Lck64-509 Y394, Blk, Fyn, Lyn and Csk, respectively). Only minimally affects the activities of other kinases (IC50 = 3.2 µM, > 33 µM, > 50 µM and > 50 µM for EGFR, PKC, CDC2/B and ZAP-70, respectively). Also shown to potently block T-cell receptor-stimulated IL-2 production in vitro (IC50 < 1-40 nM in Jurkat T cells) and in vivo (ED50 = 4 mg/kg in mice, ip.)
Catalogue Number428205
Brand Family Calbiochem®
Synonyms4-Amino-5-(4-phenoxyphenyl)-7H-pyrrolo[3,2-d]pyrimidin-7-yl-cyclopentane
References
ReferencesBurchat, A.F., et al. 2000. Bioorg. Med. Chem. Lett. 10, 2171.
Arnold. L.D., et al. 2000. Bioorg. Med. Chem. Lett. 10, 2167.
Product Information
CAS number213743-31-8
ATP CompetitiveY
FormWhite solid
Hill FormulaC₂₃H₂₂N₄O
Chemical formulaC₂₃H₂₂N₄O
ReversibleY
Structure formula ImageStructure formula Image
Quality LevelMQ100
Biological Information
Primary TargetLck₆₄₋₅₀₉ Y³⁹⁴
Primary Target IC<sub>50</sub>At5 µM ATP = < 1 nM, 2 nM, 70 nM, 1.57 µM and 1.98 µM for lck64-509 Y394, Lckcd pY394, Src, Kdr and Tie-2, respectively; IC50 at 1 mM ATP = 16 µM, 66 nM, 126 nM, 420 nM and 5.18 µM for Lck64-509 Y394, Blk, Fyn, Lyn and Csk
Purity≥95% by HPLC
Physicochemical Information
Cell permeableY
Storage and Shipping Information
Ship Code Ambient Temperature Only
Toxicity Harmful
Storage +2°C to +8°C
Protect from Light Protect from light
Do not freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Packaging Information
Packaged under inert gas Packaged under inert gas
Global Trade Item Number
Catalogue Number GTIN
428205-1MG 04055977210071